ChEMBL ligand: CHEMBL28324 (KN-62)
calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7] There should be some charts here, you may need to enable JavaScript!
calcium/calmodulin-dependent protein kinase II delta subunit/CaM kinase II delta in Human [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] There should be some charts here, you may need to enable JavaScript!
P2X7 purinoceptor in Dog [ChEMBL: CHEMBL3600277] [UniProtKB: Q64F92] There should be some charts here, you may need to enable JavaScript!
P2X purinoceptor in Guinea pig [ChEMBL: CHEMBL3600276] [UniProtKB: A9QW74] There should be some charts here, you may need to enable JavaScript!
P2X4/P2X purinoceptor 4 in Human [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571] There should be some charts here, you may need to enable JavaScript!
P2X7/P2X purinoceptor 7 in Human [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572] P2X7/P2X purinoceptor 7 in Rat [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663] There should be some charts here, you may need to enable JavaScript!
Calmodulin-dependent kinase II in Human [GtoPdb: 1554] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
calcium/calmodulin-dependent protein kinase II alpha subunit/CaM kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
ChEMBL	Inhibition of human CaMKIIalpha using calmodulin and syntide-2 incubated for 15 mins by ELISA	B	5.99	pIC50	1030	nM	IC50	J Med Chem (2020) 63: 1313-1327 [PMID:31972088]
calcium/calmodulin-dependent protein kinase II delta subunit/CaM kinase II delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557]
ChEMBL	Inhibition of human recombinant CAMK2delta using tetramethylbenzidine as substrate by spectrophotometry analysis	B	6.42	pIC50	380	nM	IC50	Bioorg Med Chem (2012) 20: 377-400 [PMID:22112539]
P2X7 purinoceptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3600277] [UniProtKB: Q64F92]
ChEMBL	Inhibition of dog P2X7 receptor	B	8	pIC50	10	nM	IC50	Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
P2X purinoceptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3600276] [UniProtKB: A9QW74]
ChEMBL	Inhibition of guinea pig P2X7 receptor	B	6.89	pIC50	130	nM	IC50	Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571]
ChEMBL	Antagonist activity against recombinant human P2X purinoceptor 4 (P2X4)	F	4	pEC50	100000	nM	EC50	J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence assay	B	4.02	pIC50	96000	nM	IC50	Bioorg Med Chem Lett (2017) 27: 759-763 [PMID:28126517]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced fluorescent ethidium accumulation	F	6.47	pIC50	340	nM	IC50	Bioorg Med Chem Lett (2009) 19: 954-958 [PMID:19110420]
ChEMBL	Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced pore formation	F	6.52	pIC50	300	nM	IC50	Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence analysis	F	6.55	pIC50	280	nM	IC50	J Med Chem (2012) 55: 3687-3698 [PMID:22400713]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium ion uptake after 2 hrs	B	6.6	pIC50	250	nM	IC50	Eur J Med Chem (2015) 106: 180-193 [PMID:26547056]
ChEMBL	Antagonist activity at recombinant human P2X7 receptor assessed as inhibition of BzATP-mediated Yo-Pro uptake measured for 1 hr by FLIPR assay	B	6.68	pIC50	210	nM	IC50	Eur J Med Chem (2013) 70: 811-830 [PMID:24246730]
ChEMBL	Antagonist activity at human purinergic P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake	F	6.76	pIC50	175	nM	IC50	Bioorg Med Chem Lett (2008) 18: 571-575 [PMID:18078749]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake after 2 hrs by fluorescence assay relative to control	B	6.8	pIC50	158	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
ChEMBL	Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake	B	6.8	pIC50	158	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced accumulation of ethidium+ after 120 mins by fluorescence assay	B	6.8	pIC50	158	nM	IC50	Eur J Med Chem (2013) 70: 811-830 [PMID:24246730]
ChEMBL	Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced ethidium ion uptake preincubated for 5 mins followed by ATP addition and incubated further 2 mins prior to ethidium addition measured up to 5 mins by flow cytometric analysis	B	6.8	pIC50	158	nM	IC50	Eur J Med Chem (2015) 106: 180-193 [PMID:26547056]
ChEMBL	Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromide uptake after 2 hrs by fluorescence assay	B	6.8	pIC50	158	nM	IC50	J Med Chem (2015) 58: 2114-2134 [PMID:25597334]
ChEMBL	Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA	B	6.84	pIC50	143	nM	IC50	J Med Chem (2015) 58: 2114-2134 [PMID:25597334]
ChEMBL	Antagonist activity at P2X7 in LPS/IFN gamma differentiated human THP-1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP stimulation for 30 mins by ELISA	B	6.89	pIC50	130	nM	IC50	Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
ChEMBL	Antagonist activity at P2X7 receptor expressed in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta production after 4 hrs by ELISA	B	6.89	pIC50	129	nM	IC50	Eur J Med Chem (2015) 106: 180-193 [PMID:26547056]
ChEMBL	Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzATP challenge measured after 30 mins by ELISA	F	6.92	pIC50	120	nM	IC50	J Med Chem (2012) 55: 3687-3698 [PMID:22400713]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced fluorescent ethidium accumulation at 10 uM	F	6.96	pIC50	110	nM	IC50	Bioorg Med Chem Lett (2009) 19: 6053-6058 [PMID:19800793]
ChEMBL	Inhibition of human P2X7 receptor	B	7	pIC50	100	nM	IC50	Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
ChEMBL	Antagonist activity at P2X7 receptor (unknown origin)	B	7.03	pIC50	94.4	nM	IC50	Bioorg Med Chem (2014) 22: 54-88 [PMID:24314880]
ChEMBL	Antagonistic activity against P2X7 receptor measured as the ATP dependent calcium influx in human monocytes	F	7.29	pIC50	51.1	nM	IC50	J Med Chem (2003) 46: 1318-1329 [PMID:12672232]
ChEMBL	Antagonist activity at human P2X7 receptor	B	7.29	pIC50	51	nM	IC50	J Med Chem (2015) 58: 2114-2134 [PMID:25597334]
ChEMBL	Antagonistic activity against P2X7 receptor	F	7.29	pIC50	51	nM	IC50	Bioorg Med Chem Lett (2003) 13: 4047-4050 [PMID:14592505]
ChEMBL	Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium influx	F	7.3	pIC50	50.12	nM	IC50	J Med Chem (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL	Inhibitory concentration was evaluated against P2X purinoceptor 7	B	7.87	pIC50	13.4	nM	IC50	Bioorg Med Chem Lett (2000) 10: 681-684 [PMID:10762053]
ChEMBL	Antagonist activity at P2X7 receptor in human lymphocytes assessed as inhibition of ATP-induced Ba2+ influx	F	7.9	pIC50	12.59	nM	IC50	J Med Chem (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL	Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA	B	7.9	pIC50	12.59	nM	IC50	J Med Chem (2015) 58: 2114-2134 [PMID:25597334]
ChEMBL	Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7)	F	7.47	pEC50	34	nM	EC50	J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663]
ChEMBL	Inhibition of rat P2X7 receptor	B	4	pIC50	>100000	nM	IC50	Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
Calmodulin-dependent kinase II in Human [GtoPdb: 1554]
GtoPdb	-	-	6.05	pIC50	900	nM	IC50	J Biol Chem (1990) 265: 4315-20 [PMID:2155222]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]